2. Immunology/Inflammation
  3. PGE synthase
  4. CAY10526

CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1.

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CAY10526 Chemical Structure

CAY10526 Chemical Structure

CAS No. : 938069-71-7

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1[1].

Molecular Weight

311.15

Formula

C12H7BrO3S
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1C(Br)=C(C(O1)O)C2=CC3=CC=CC=C3S2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (214.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2139 mL 16.0694 mL 32.1388 mL
5 mM 0.6428 mL 3.2139 mL 6.4278 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.03 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2139 mL 16.0694 mL 32.1388 mL 80.3471 mL
5 mM 0.6428 mL 3.2139 mL 6.4278 mL 16.0694 mL
10 mM 0.3214 mL 1.6069 mL 3.2139 mL 8.0347 mL
15 mM 0.2143 mL 1.0713 mL 2.1426 mL 5.3565 mL
20 mM 0.1607 mL 0.8035 mL 1.6069 mL 4.0174 mL
25 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2139 mL
30 mM 0.1071 mL 0.5356 mL 1.0713 mL 2.6782 mL
40 mM 0.0803 mL 0.4017 mL 0.8035 mL 2.0087 mL
50 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6069 mL
60 mM 0.0536 mL 0.2678 mL 0.5356 mL 1.3391 mL
80 mM 0.0402 mL 0.2009 mL 0.4017 mL 1.0043 mL
100 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8035 mL
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CAY10526 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CAY10526938069-71-7CAY 10526CAY-10526PGE synthaseProstaglandin E synthasemicrosomal PGE2 synthase-1mPGES1 inhibitorPGE2 productionincreases apoptosismelanoma xenograftsreduces BCL-2 and BCL-XL anti-apoptoticincreases BAX and BAKpro-apoptoticcleaved caspase 3A375SB2WM793Inhibitorinhibitorinhibit

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